Bollettino chimico farmaceutico最新文献

Carbopol 941 (C-941), a bioadhesive polymer and theobroma oil (TEO) were used in the formulation of melt extrusion bioadhesive tablets (MEBT) of diclofenac (DC). Different batches of the MEBT were formulated using different combinations of C-941 granules containing DC and TEO. The bioadhesive properties of the tablets were studied using a tensiometer by measuring the bioadhesive strength generated when the tablet interacts with the mucus of everted hog jejunum. Some physical properties of the tablets evaluated were weight uniformity, crushing strength, friability, tablet thickness and diameter liquefaction time and absolute drug content. Release of DC from the MEBT was carried out in simulated intestinal fluid (SIF), pH 7.2. The tablets had low liquefaction times and were highly bioadhesive. Result of the study indicated that TEO could be used in the formulation of MEBT of DC granulated with C-941 for prolonged and controlled delivery of DC.

Isolation and properties of glycosylated pig prolactin (G-PRL)--Crude prolacting was received via extraction from lyophilized hypophyses with acidic 70% acetone, and then by protein precipitation via increasing acetone concentration in the extract to 92%. Received precipitate was dissolved in 0.1 M acetic acid and prolactin was precipitated in the isoelectric point at the pH = 4.97. Prolactin precipitate was dissolved in phosphate buffer pH = 7.50 and adsorbed on the DEAE-Sephadex column, and then eluated with linear gradient at NaCl concentration range 0.00-0.40 M. Prolactin with molecular mass 24.0 kD was eluated at NaCl concentration 0.19-0.25 M. Using gel filtration method on Sephadex G-100 glycosylated prolactin was divided into 2 fractions with molecular mass equal--55.8 and 17.4 kD. Both 24.0 kD--prolactin and its glycosylated form were characterized by high biological activity. Glycosylated prolactin contains among others mannose and fucose.

This paper presents the application of the regression analysis program and the program for comparing linear regressions (modified method for one-way, analysis of variance), writtens in BASIC program language, for instance, determination of content of Diclofenac-Sodium (active ingredient in DIKLOFEN injections, ampules á 75 mg/3 ml). Stability testing of Diclofenac-Sodium was done by isothermic method of accelerated aging at 4 different temperatures (30 degrees, 40 degrees, 50 degrees and 60 degrees C) as a function of time (4 different duration of treatment: (0-155, 0-145, 0-74 and 0-44 days). The decrease in stability (decrease in the mean value of the content of Diclofenac-Sodium (in %), at different temperatures as a function of time, is possible to describe by, linear dependance. According to the value for regression equation values, the times are assessed in which the content of Diclofenac-Sodium (in %) will decrease by 10%, of the initial value. The times are follows at 30 degrees C 761.02 days, at 40 degrees C 397.26 days, at 50 degrees C 201.96 days and at 60 degrees C 58.85 days. The estimated times (in days) in which the mean value for Diclofenac-Sodium content (in %) will by 10% of the initial values, as a junction of time, are most suitably described by 3rd order parabola. Based on the parameter values which describe the 3rd order parabola, the time was estimated in which Diclofenac-Sodium content mean value (in %) will fall by 10% of the initial one at average ambient temperatures of 20 degrees C and 25 degrees C. The times are: 1409.47 days (20 degrees C) and 1042.39 days (25 degrees C). Based on the value for Fischer's coefficien (F), the comparison of trenf of Diclofenac-Sodium content (in %) shows that, under the influence of different temperatures as a function of time, among them, depending on temperature value, there is: statistically very significant difference (P << .05) at 50 degrees C and lower toward 60 degrees C, i.e. statistically probably significant difference (P > 0.01) at 40 degrees C and lower towards 50 degrees C and there is no statistically significance difference (P >> 0.05) at 30 degrees C towards 40 degrees C.

The influence of magnesium concentration and salt form on the absorption of this element in the rat small intestine was investigated. The following magnesium salts were studied: gluconate, fumarate, and chloride. At 1 and 5 mM concentrations absorption was most efficient from gluconate whereas at 10 mM absorption from fumrate was more efficient. Mg2+ absorption half-life (t50%) varied with salt and concentration. The Mg2+ absorption half-life for magnesium gluconate at 10 mM concentration was 42 times as long as at 1 mM concentration. The biggest area under the curve, which characterizes substance bioavailability, was observed for each of the investigated salts at 5 mM. Therefore, we may conclude that magnesium administration at 5 mM concentration would be optimal.

Four previously stynthesized derivatives of 3- (4-benzyl-1-piperazinyl)-1-phenylpropanol were screened for analgesic activity in albino mice using a variation of the Eddy and Lambach hot plate method. The result showed that the most significant analgesic effect was elicited by the parent secondary 3-piperazinylpropanol, namely 3-(4-benzyl-1-piperazinyl)-1-phenylpropanol. Its esterification products with propanoyl, benzoyl and phenylacetyl chlorides exhibited reduced analgesic properties. The percent maximum protection against thermal pain produced by Aspirin (71.43%) was twice as high as that produced by the most active of the four derivatives (43.65%). The analgesic effect of the compounds was dose dependent. From acute toxicity studies in mice, the LD50 values were estimated to be in range of moderate toxicity (89.74 to 243 mg/kg). The most active of the compounds studied, namely, 3-(4-benzyl-1-piperazinyl-1-phenylpropanols, was also found to be the most toxic. The margin between its safe doses and its LD50 (89.74 mg/kg) was found to be very narrow. Esterification of the 3-(4-benzyl-1-piperazinyl)-1-phenylpropanol led to decrease in its analgesic activity and also a decrease in its toxicity.

Some 9-(substituted with heteroaryl)-phenanthrene compounds, polycyclic aromatic hydrocarbons (PAH), were obtained by two different methods. In the first method, 9-phenanthraldehyde was reacted with some dion compounds such as benzil, toluil, anisil, etc in the presence of ammonium acetate and glacial acetic acid. In the second method, 9-phenanthraldehyde was reacted with 5-substituted-1,2-phenylenediamine derivatives in the presence of NaHSO3 and ethanol. All of synthesized compounds by us were original and these compounds have not been studied in literature so far. The structures of compounds were confirmed by spectral data and elemental analyses results. The effects of compounds were studied on intracellular calcium level. All of the compounds were examined between the concentrations of 1 and 0.5 microg/mL.